N-(2-(difluoromethoxy)-5-methylphenyl)-4-methoxy-3-(piperazin-1-yl)benzenesulfonamide | 1253909-27-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N-(2-(difluoromethoxy)-5-methylphenyl)-4-methoxy-3-(piperazin-1-yl)benzenesulfonamide
• 英文别名: N-[2-(difluoromethoxy)-5-methylphenyl]-4-methoxy-3-piperazin-1-ylbenzenesulfonamide
• CAS: 1253909-27-1
• 化学式: C₁₉H₂₃F₂N₃O₄S
• 分子量: 427.472
• InChiKey: UKWJMLAKMBXCII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  88.3
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  聚合甲醛 、 N-(2-(difluoromethoxy)-5-methylphenyl)-4-methoxy-3-(piperazin-1-yl)benzenesulfonamide 在 三乙酰氧基硼氢化钠 、 溶剂黄146 、 水 作用下， 以 二氯甲烷 为溶剂， 反应 72.17h， 生成 N-(2-difluoromethoxy-5-methylphenyl)-4-methoxy-3-(4-methylpiperazin-1-yl)benzenesulfonamide hydrochloride
  参考文献：
  名称：

  [EN] N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
  [FR] COMPOSÉS N-PHÉNYL-(PIPÉRAZINYL OU HOMOPIPÉRAZINYL)- BENZÈNESULFONAMIDE OU BENZÈNESULFONYL-PHÉNYL-(PIPÉRAZINE OU HOMOPIPÉRAZINE) ADAPTÉS AU TRAITEMENT DE TROUBLES RÉPONDANT À LA MODULATION DU RÉCEPTEUR 5-HT6 DE LA SÉROTONINE

  摘要：

  本发明涉及N-苯基-(哌嗪基或同源哌嗪基)-苯磺酰胺或苯磺酰基-苯基-(哌嗪或同源哌嗪)化合物，含有它们的药物组合物，以及它们在治疗中的应用。这些化合物具有有价值的治疗特性，特别适用于治疗对5-羟色胺5-HT6受体调节有响应的疾病。其中X是键或基团N-R4；R1是氢或甲基；R2是氢或甲基；R3是氢，C1-C3烷基，氟，C1-C2烷氧基或氟代C1-C2烷氧基；R4是氢，C1-C4烷基，C3-C4环烷基，或C3-C4环烷基-CH2-；R5是氢，氟，氯，C1-C2烷基，氟代C1-C2烷基，C1-C2烷氧基或氟代C1-C2烷氧基；R6是氢，氟或氯；n为1或2。

  公开号：

  WO2010125134A1

文献信息

• N-PHENYL- (PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
  申请人：Haupt Andreas

  公开号：US20100280014A1

  公开（公告）日：2010-11-04

  The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. wherein X is a bond or a group N—R 4 ; R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, C 1 -C 3 alkyl, fluorine, C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 4 is hydrogen, C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl, or C 3 -C 4 cycloalkyl-CH 2 —; R 5 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl, fluorinated C 1 -C 2 alkyl, C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 6 is hydrogen, fluorine or chlorine; and n is 1 or 2.

  本发明涉及N-苯基-(哌嗪基或同源哌嗪基)-苯磺酰胺或苯磺酰基苯基-(哌嗪或同源哌嗪)化合物、含有它们的制药组合物以及它们在治疗中的应用。该化合物具有有价值的治疗特性，特别适用于治疗对5-羟色胺5-HT6受体调节有反应的疾病。其中，X是键或N-R4基团；R1是氢或甲基；R2是氢或甲基；R3是氢、C1-C3烷基、氟、C1-C2烷氧基或氟代C1-C2烷氧基；R4是氢、C1-C4烷基、C3-C4环烷基或C3-C4环烷基-CH2-；R5是氢、氟、氯、C1-C2烷基、氟代C1-C2烷基、C1-C2烷氧基或氟代C1-C2烷氧基；R6是氢、氟或氯；n为1或2。
• N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
  申请人：Haupt Andreas

  公开号：US20120040969A1

  公开（公告）日：2012-02-16

  The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor.

  本发明涉及N-苯基-(哌嗪基或同型哌嗪基)-苯磺酰胺或苯磺酰基苯基-(哌嗪或同型哌嗪)化合物，含有它们的制药组合物以及它们在治疗中的应用。这些化合物具有有价值的治疗特性，特别适用于治疗对5-HT6受体调节有反应的疾病。
• N-phenyl- (piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
  申请人：Abbott GmbH & Co. KG

  公开号：US08076326B2

  公开（公告）日：2011-12-13

  The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein X is a bond or a group N—R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3 alkyl, fluorine, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 cycloalkyl-CH2—; R5 is hydrogen, fluorine, chlorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R6 is hydrogen, fluorine or chlorine; and n is 1 or 2.

  本发明涉及N-苯基-(哌嗪基或同型哌嗪基)-苯磺酰胺或苯磺酰基苯基-(哌嗪或同型哌嗪)化合物，含有它们的药物组合物以及它们在治疗中的使用。这些化合物具有有价值的治疗性能，特别适用于治疗对5-HT6受体调节有响应的疾病。 其中， X是键或N—R4基团； R1是氢或甲基； R2是氢或甲基； R3是氢、C1-C3烷基、氟、C1-C2烷氧基或氟化C1-C2烷氧基； R4是氢、C1-C4烷基、C3-C4环烷基或C3-C4环烷基-CH2—； R5是氢、氟、氯、C1-C2烷基、氟化C1-C2烷基、C1-C2烷氧基或氟化C1-C2烷氧基； R6是氢、氟或氯； n为1或2。
• N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
  申请人：Abbott GmbH & Co. KG

  公开号：US08343959B2

  公开（公告）日：2013-01-01

  The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.

  本发明涉及N-苯基-(哌嗪基或同型哌嗪基)-苯磺酰胺或苯磺酰基苯基-(哌嗪或同型哌嗪)化合物、包含它们的制药组合物以及它们在治疗中的应用。这些化合物具有有价值的治疗性能，特别适用于治疗对5-HT6受体调节有反应的疾病。
• N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR& xA;
  申请人：Abbott GmbH & Co. KG

  公开号：EP2432769A1

  公开（公告）日：2012-03-28